孕烯醇酮D环结构修饰的合成方法及生物活性研究进展  

Progress in Synthetic Methods and Biological Activities of Pregnenolone D-ring Structural Modifications

作　　者：董远 马养民[1] 马思悦 DONG Yuan;MA Yangmin;MA Siyue(Key Laboratory of Chemical Additives for China National Light Industry,Ministry of Education,College of Chemistry&Chemical Engineering,Shaanxi University of Science&Technology,Xi'an 710021,China)

机构地区：[1]陕西科技大学化学与化工学院中国轻工业轻化工助剂重点实验室,陕西西安710021

出　　处：《广州化学》2024年第2期16-23,I0002,共9页Guangzhou Chemistry

基　　金：国家自然科学基金(No.22178205);陕西省重点研发计划(2022GY-203);中国博士后基金(2022M711994)。

摘　　要：简单介绍了甾体的结构以及在医药方面的广泛应用;阐述了16-脱氢孕烯醇酮醋酸酯(16-DPA)作为合成甾体药物的关键中间体在甾体合成中占有重要地位;随后详细综述了以不同基团修饰16-DPA的D环得到甾体衍生物的合成方法,其中包括N杂环(噁唑环、吡唑环、嘧啶环、咪唑环)、O杂环、碳环等修饰;以及其显示的抗肿瘤抗炎等生物活性进行分析;最后进行总结并对其发展趋势和应用前景进行了展望。The structure of steroids and their wide range of applications in medicine are briefly described.Firstly,it is elaborated that 16-dehydropregnenolone acetate(16-DPA)occupies an important position in steroid synthesis as a key intermediate in the synthesis of steroid drugs.Subsequently,the synthetic methods of modifying the D-ring of 16-DPA with different groups to obtain steroid derivatives are reviewed in detail,including N-heterocyclic(oxazole,pyrazole,pyrimidine,and imidazole),O-heterocyclic,carbocyclic,and other modifications.As well as their displayed biological activities such as anti-tumor and anti-inflammatory are analyzed.Finally,it is summarized and its development trend and application prospects are outlooked.

关 键 词：16-DPA 孕烯醇酮 位点修饰 甾体 抗肿瘤活性 

分 类 号：O629.2[理学—有机化学]